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Assay Detail

CHEMBL5731402

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Binding
KINOMEscan Enzyme Binding Assays: Kinase enzyme binding affinities of compounds disclosed herein were determined using the KINOMEscan technology performed by DiscoveRx Corporation, San Diego, Calif., USA (www.kinomescan.com).
ChEMBL ↗
306
Total Activities
91
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (CHEMBL3130) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazopyridazine derivatives as PI3KB inhibitors
(2018)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 102 6.86 8.30
kon 102 - -
k_off 102 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6061149 — — 3 8.30
CHEMBL5989927 — — 3 8.05
CHEMBL5799166 — — 6 8.05
CHEMBL5803247 — — 3 7.96
CHEMBL3983623 — — 3 7.96
CHEMBL6034062 — — 3 7.92
CHEMBL5812386 — — 3 7.82
CHEMBL5894050 — — 3 7.80
CHEMBL5988647 — — 3 7.77
CHEMBL3956037 — — 3 7.70
CHEMBL5831673 — — 3 7.55
CHEMBL5930691 — — 9 7.51
CHEMBL6001051 — — 3 7.51
CHEMBL5807461 — — 3 7.48
CHEMBL5803568 — — 3 7.47
CHEMBL5924926 — — 3 7.47
CHEMBL5929842 — — 3 7.46
CHEMBL3955003 — — 3 7.40
CHEMBL6037249 — — 3 7.38
CHEMBL5990201 — — 3 7.36
CHEMBL5925644 — — 3 7.33
CHEMBL5850080 — — 3 7.33
CHEMBL3974658 — — 3 7.32
CHEMBL5888478 — — 6 7.32
CHEMBL5880092 — — 6 7.31
CHEMBL5781447 — — 3 7.25
CHEMBL6018580 — — 3 7.25
CHEMBL5810486 — — 6 7.24
CHEMBL5842791 — — 3 7.24
CHEMBL6064382 — — 3 7.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6061149 — Kd = 5.0 nM 8.30
CHEMBL5989927 — Kd = 9.0 nM 8.05
CHEMBL5799166 — Kd = 9.0 nM 8.05
CHEMBL5803247 — Kd = 11.0 nM 7.96
CHEMBL3983623 — Kd = 11.0 nM 7.96
CHEMBL6034062 — Kd = 12.0 nM 7.92
CHEMBL5812386 — Kd = 15.0 nM 7.82
CHEMBL5894050 — Kd = 16.0 nM 7.80
CHEMBL5799166 — Kd = 16.0 nM 7.80
CHEMBL5988647 — Kd = 17.0 nM 7.77
CHEMBL3956037 — Kd = 20.0 nM 7.70
CHEMBL5831673 — Kd = 28.0 nM 7.55
CHEMBL5930691 — Kd = 31.0 nM 7.51
CHEMBL6001051 — Kd = 31.0 nM 7.51
CHEMBL5807461 — Kd = 33.0 nM 7.48
CHEMBL5924926 — Kd = 34.0 nM 7.47
CHEMBL5803568 — Kd = 34.0 nM 7.47
CHEMBL5929842 — Kd = 35.0 nM 7.46
CHEMBL5930691 — Kd = 35.0 nM 7.46
CHEMBL3955003 — Kd = 40.0 nM 7.40
CHEMBL6037249 — Kd = 42.0 nM 7.38
CHEMBL5990201 — Kd = 44.0 nM 7.36
CHEMBL5850080 — Kd = 47.0 nM 7.33
CHEMBL5925644 — Kd = 47.0 nM 7.33
CHEMBL5930691 — Kd = 47.0 nM 7.33
CHEMBL5888478 — Kd = 48.0 nM 7.32
CHEMBL3974658 — Kd = 48.0 nM 7.32
CHEMBL5880092 — Kd = 49.0 nM 7.31
CHEMBL6018580 — Kd = 56.0 nM 7.25
CHEMBL5781447 — Kd = 56.0 nM 7.25
CHEMBL5842791 — Kd = 58.0 nM 7.24
CHEMBL5810486 — Kd = 58.0 nM 7.24
CHEMBL6064382 — Kd = 59.0 nM 7.23
CHEMBL5826253 — Kd = 62.0 nM 7.21
CHEMBL5964364 — Kd = 69.0 nM 7.16
CHEMBL5889612 — Kd = 69.0 nM 7.16
CHEMBL5781910 — Kd = 71.0 nM 7.15
CHEMBL5810941 — Kd = 73.0 nM 7.14
CHEMBL5858003 — Kd = 74.0 nM 7.13
CHEMBL5872858 — Kd = 75.0 nM 7.12
CHEMBL5860050 — Kd = 75.0 nM 7.12
CHEMBL6065963 — Kd = 80.0 nM 7.10
CHEMBL5880092 — Kd = 81.0 nM 7.09
CHEMBL6049412 — Kd = 83.0 nM 7.08
CHEMBL5749126 — Kd = 85.0 nM 7.07
CHEMBL5963673 — Kd = 98.0 nM 7.01
CHEMBL5903970 — Kd = 105.0 nM 6.98
CHEMBL5783879 — Kd = 105.0 nM 6.98
CHEMBL6050387 — Kd = 117.0 nM 6.93
CHEMBL5888478 — Kd = 120.0 nM 6.92